Assay Detail
Functional
CHEMBL4047708
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human P2Y2R expressed in human Jurkat cells assessed as inhibition of UTP-activated intracellular calcium mobilization by fluo-3AM dye based fluorescence assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 28 | 6.60 | 8.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4066222 | — | — | 1 | 8.50 |
| CHEMBL4086462 | — | — | 1 | 8.00 |
| CHEMBL4090014 | — | — | 1 | 7.90 |
| CHEMBL4082045 | — | — | 1 | 7.80 |
| CHEMBL4084674 | — | — | 1 | 7.80 |
| CHEMBL4073600 | — | — | 1 | 7.70 |
| CHEMBL4089252 | — | — | 1 | 7.60 |
| CHEMBL4068069 | — | — | 1 | 7.50 |
| CHEMBL4099908 | — | — | 1 | 7.40 |
| CHEMBL4065010 | — | — | 1 | 7.30 |
| CHEMBL4094225 | — | — | 1 | 7.20 |
| CHEMBL4081384 | — | — | 1 | 7.20 |
| CHEMBL4063008 | — | — | 1 | 7.10 |
| CHEMBL4105209 | — | — | 1 | 7.00 |
| CHEMBL4080964 | — | — | 1 | 6.70 |
| CHEMBL4081909 | — | — | 1 | 6.60 |
| CHEMBL4061969 | — | — | 1 | 6.00 |
| CHEMBL4067621 | — | — | 1 | 5.90 |
| CHEMBL4096541 | — | — | 1 | 5.80 |
| CHEMBL4088846 | — | — | 1 | 5.70 |
| CHEMBL4067715 | — | — | 1 | 5.70 |
| CHEMBL4070330 | — | — | 1 | 5.60 |
| CHEMBL4087442 | — | — | 1 | 5.60 |
| CHEMBL4105297 | — | — | 1 | 5.40 |
| CHEMBL4095137 | — | — | 1 | 5.40 |
| CHEMBL4097505 | — | — | 1 | 5.20 |
| CHEMBL4078610 | — | — | 1 | 4.70 |
| CHEMBL4078514 | — | — | 1 | 4.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4066222 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL4086462 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL4090014 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL4082045 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL4084674 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL4073600 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL4089252 | — | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL4068069 | — | Kd | = | 31.62 | nM | 7.50 |
| CHEMBL4099908 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL4065010 | — | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL4094225 | — | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL4081384 | — | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL4063008 | — | Kd | = | 79.43 | nM | 7.10 |
| CHEMBL4105209 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL4080964 | — | Kd | = | 199.53 | nM | 6.70 |
| CHEMBL4081909 | — | Kd | = | 251.19 | nM | 6.60 |
| CHEMBL4061969 | — | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL4067621 | — | Kd | = | 1258.93 | nM | 5.90 |
| CHEMBL4096541 | — | Kd | = | 1584.89 | nM | 5.80 |
| CHEMBL4088846 | — | Kd | = | 1995.26 | nM | 5.70 |
| CHEMBL4067715 | — | Kd | = | 1995.26 | nM | 5.70 |
| CHEMBL4070330 | — | Kd | = | 2511.89 | nM | 5.60 |
| CHEMBL4087442 | — | Kd | = | 2511.89 | nM | 5.60 |
| CHEMBL4105297 | — | Kd | = | 3981.07 | nM | 5.40 |
| CHEMBL4095137 | — | Kd | = | 3981.07 | nM | 5.40 |
| CHEMBL4097505 | — | Kd | = | 6309.57 | nM | 5.20 |
| CHEMBL4078610 | — | Kd | = | 19952.62 | nM | 4.70 |
| CHEMBL4078514 | — | Kd | = | 39810.72 | nM | 4.40 |